DSRM-3716 (5-Iodoisoquinoline) 是一种有效的选择性 SARM1 NADase 抑制剂，IC₅₀ 为 75 nM。DSRM-3716 对其他 NAD⁺ 加工酶、受体和转运蛋白具有选择性。DSRM-3716 具有强大的轴突保护作用。

DSRM-3716 (5-Iodoisoquinoline) is a potent and selective SARM1 NADase inhibitor with an IC 50 of 75 nM. DSRM-3716 is selective against other NAD-processing enzymes, receptors, and transporters. DSRM-3716 provides robust axon protection.

Solid

IC50: 75 nM (SARM1 NADase)

DSRM-3716 treatment produces dose-dependent inhibition of cADPR increase (IC50 of 2.8 μM) and substantial preservation of NAD in these cultures in a manner consistent with engagement and inhibition of SARM1 enzymatic NADase activity inside the cells.
DSRM-3716 prevents neurofilament light chain (NfL) release from severed axons in a dose-dependent manner, with an IC50 of ~2 μM.
The potency of DSRM-3716 to inhibit cADPR increase caused by axotomy (IC50 of 2.8 μM) is similar to the potency required to prevent axonal degeneration (IC50 of 2.1 μM).
DSRM-3716 inhibits the SARM1-dependent cell destruction pathway triggered by Rotenone in sensory neurons. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Robert O Hughes, et al. Small Molecule SARM1 Inhibitors Recapitulate the SARM1 -/- Phenotype and Allow Recovery of a Metastable Pool of Axons Fated to Degenerate. Cell Rep. 2021 Jan 5;34(1):108588.

In Vitro: DMSO : 50 mg/mL (196.03 mM; Need ultrasonic)配制储备液